Synthesis of benzamide derivatives as TRPV1 antagonists
| Autor: | Yoshihito Kanai, Shimojo Masato, Ayako Iki-Taki, Fumitaka Ito, Tetsuya Tamura, Takafumi Ikeda, Madoka Jinno, Naoya Makita, Masaki Sudo, Yuji Shishido, Takashi Ohmi, Atsuko Ohta |
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| Rok vydání: | 2008 |
| Předmět: |
Tryptamine
Stereochemistry High-throughput screening Clinical Biochemistry TRPV1 TRPV Cation Channels Pharmaceutical Science Biochemistry Chemical synthesis Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Combinatorial Chemistry Techniques Humans Benzamide Molecular Biology Indole test Analgesics Molecular Structure Organic Chemistry Antagonist Rats chemistry Benzamides Molecular Medicine Bioisostere |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 18:1072-1078 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.12.007 |
| Popis: | From hit compounds identified by high throughput screening (HTS), we have found compound 1 as a lead TRPV1 antagonist and confirmed its potential as a treatment for pain. Compound 1 has led to potent TRPV1 antagonistic benzamide derivatives ((±)-2: human IC50 = 23 nM, (±)-3: human IC50 = 14 nM in the capsaicin-induced calcium influx assay) containing indole and naphthyl moieties, obtained by elaboration of the tryptamine scaffold or via bioisosteric replacements. |
| Databáze: | OpenAIRE |
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